GHSR Agonist

Anamorelin (RC-1291) is an orally active Ghrelin receptor agonist with an EC₅₀ of 0.74 nM. Anamorelin can promote appetite, increase body weight, and stimulate the secretion of growth hormone and insulin-like growth factor-1. Anamorelin can be used in the research of anorexia and cancer cachexia.

Ibutamoren Mesylate (MK-677) is a potent, non-peptide Growth hormone secretagogue receptor (GHSR) agonist. Ibutamoren Mesylate is an orally active growth hormone (GH) secretagogue.

Anamorelin (RC-1291) hydrochloride is an orally active Ghrelin receptor agonist with an EC₅₀ of 0.74 nM. Anamorelin hydrochloride can promote appetite, increase body weight, and stimulate the secretion of growth hormone and insulin-like growth factor-1. Anamorelin hydrochloride can be used in the research of anorexia and cancer cachexia.

KARI 101 is a blood-brain barrier permeable acid sphingomyelinase (ASM) inhibitor. KARI 101 directly inhibits ASM activity and reduces ceramide production. KARI 101 induces Ca²⁺ mobilization, activates AMPK and triggers GHSR1α internalization. KARI 101 can be used for the research of Alzheimer's disease.

Ibutamoren (MK-677 free base; MK-0677 free base) is an orally active non-peptide growth hormone secretagogue receptor agonist. Ibutamoren activates signal cascades by mimicking endogenous ligands, triggers pulsatile release of growth hormone from the pituitary gland, and increases serum levels of IGF-1 and insulin-like growth factor-binding protein 3. Ibutamoren not only increases the frequency of growth hormone pulses in male individuals, but also promotes elevated bone formation markers in female individuals with postmenopausal osteoporosis. The combination of Ibutamoren with Alendronate sodium hydrate (HY-11101) significantly increases bone mineral density at the femoral neck. However, Ibutamoren may cause mild, reversible adverse reactions such as increased appetite, fluid retention, and elevated fasting blood glucose. Ibutamoren has been widely used in studies related to idiopathic growth hormone deficiency, sarcopenia, Alzheimer's disease, and osteoporosis.

Relamorelin (RM-131) TFA, a pentapeptide ghrelin analog, is a selective ghrelin/growth hormone secretagogue receptor (GHSR) agonist with a K_i of 0.42 nM for GHS-1a receptor. Relamorelin TFA is centrally penetrant. Relamorelin TFA increases growth hormone levels and accelerates gastric emptying. Relamorelin TFA has the potential for cachexia, gastroparesis, and gastric/intestinal dysmobility disorders research.

Capromorelin Tartrate is an orally active, potent growth hormone secretagogue receptor (GHSR) agonist, with K_i of 7 nM for hGHS-R1a.

Macimorelin (EP-1572) acetate, a GH secretagogue, is an orally active GHSR agonist. Macimorelin acetate stimulates GH release. Macimorelin acetate can be used in the research of adult growth hormone deficiency (AGHD), and Cancer anorexia-cachexia syndrome (CACS).

KARI 201 hydrochloride is a selective, brain penetrant pand competitive acid sphingomyelinase (ASM) inhibitor with an IC₅₀ of 338.3?nM. KARI 201 hydrochloride is a ghrelin receptor agonist. KARI 201 hydrochloride improves neuropathological features of Alzheimer's disease.

Ulimorelin (TZP-101) is a ghrelin receptor (GRLN) agonist with an EC₅₀ of 29 nM and a K_i of 16 nM. Ulimorelin is a prokinetic agent and causes vasorelaxation through competitive antagonist action at α1-adrenoceptors. Ulimorelin stimulates intestinal motility and is used for malnutrition.

L-692585 is a potent and nonpeptidyl growth hormone secretagogue receptor (GHS-R1a) agonist, with a K_i of 0.8 nM. L-692585 acts directly on somatotropes causing GH release.

GHRF, mouse TFA, a mouse growth hormone-releasing factor, is a peptide containing 44 amino acids. GHRF, mouse TFA stimulates the release and synthesis of growth hormone.

L-692429 (MK-0751) is a benzolactam derivative and a nonpeptidyl growth hormone secretagogue (GHS) agonist. L-692429 binds to G protein-coupled receptor with a K_i of 63 nM.

(D-Ala2)-GRF (1-29) amide (human) is a superagonist of GRF, exhibiting extremely high GH-releasing activity about 50 times that of GRF (1-29) in both pigs and rats.

Relamorelin (RM-131), a pentapeptide ghrelin analog, is a selective ghrelin/growth hormone secretagogue receptor (GHSR) agonist with a K_i of 0.42 nM for GHS-1a receptor. Relamorelin is centrally penetrant. Relamorelin increases growth hormone levels and accelerates gastric emptying. Relamorelin has the potential for cachexia, gastroparesis, and gastric/intestinal dysmobility disorders research.

Relamorelin (RM-131) acetate, a pentapeptide ghrelin analog, is a selective ghrelin/growth hormone secretagogue receptor (GHSR) agonist with a K_i of 0.42 nM for GHS-1a receptor. Relamorelin acetate is centrally penetrant. Relamorelin acetate increases growth hormone levels and accelerates gastric emptying. Relamorelin acetate has the potential for cachexia, gastroparesis, and gastric/intestinal dysmobility disorders research.

AZ-GHS-38 (compound 38) is an orally active CNS-penetrant inverse agonist of growth hormone secretagogue receptor (GHS-R1a) with an IC₅₀ of 6.7 nM. AZ-GHS-38 results in acute reduction of food intake in wild-type mice. AZ-GHS-38 can be used for anti-obesity research.

Ghrelin receptor full agonist-2 (compound 12j) is a highly potent Ghrelin receptor full agonist.

GSK894490A is a non-peptide ghrelin receptor agonist.

BMS-604992 (EX-1314) free base is a selective, orally active small-molecule growth hormone secretagogue receptor (GHSR) agonist. BMS-604992 free base demonstrates high-affinity binding (k_i=2.3 nM) and potent functional activity (EC₅₀=0.4 nM). BMS-604992 free base can stimulate food intake in rodents.